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Assay Detail

CHEMBL840199

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Binding
Binding affinity for human estrogen receptor alpha
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel quinoline-based estrogen receptor ligands using peptide interaction profiling.
Hoekstra WJ, Patel HS, Liang X, Blanc JB, Heyer DO, Willson TM, Iannone MA, Kadwell SH, Miller LA, Pearce KH, Simmons CA, Shearin J.
J Med Chem (2005) 48 : 2243 -2247
PubMed 15771467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.55 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 8.70
CHEMBL195515 1 8.60
CHEMBL2137046 1 8.60
CHEMBL195080 1 8.10
CHEMBL370750 1 8.00
CHEMBL194774 1 8.00
CHEMBL363630 1 7.80
CHEMBL193865 1 7.60
CHEMBL192025 1 7.00
CHEMBL370492 1 6.90
CHEMBL193730 1 5.80
CHEMBL194600 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL Ki = 1.995 nM 8.70
CHEMBL195515 Ki = 2.512 nM 8.60
CHEMBL2137046 Ki = 2.512 nM 8.60
CHEMBL195080 Ki = 7.943 nM 8.10
CHEMBL370750 Ki = 10.0 nM 8.00
CHEMBL194774 Ki = 10.0 nM 8.00
CHEMBL363630 Ki = 15.85 nM 7.80
CHEMBL193865 Ki = 25.12 nM 7.60
CHEMBL192025 Ki = 100.0 nM 7.00
CHEMBL370492 Ki = 125.89 nM 6.90
CHEMBL193730 Ki = 1584.89 nM 5.80
CHEMBL194600 Ki = 3162.28 nM 5.50